《Synthesis and Structure-Activity Relationships of 5′-Aryl-14-alkoxypyridomorphinans: Identification of a μ Opioid Receptor Agonist/δ Opioid Receptor Antagonist Ligand with Systemic Antinociceptive Activity and Diminished Opioid Side Effects》 was written by Vekariya, Rakesh H.; Lei, Wei; Ray, Abhisek; Saini, Surendra K.; Zhang, Sixue; Molnar, Gabriella; Barlow, Deborah; Karlage, Kelly L.; Bilsky, Edward J.; Houseknecht, Karen L.; Largent-Milnes, Tally M.; Streicher, John M.; Ananthan, Subramaniam. Related Products of 197958-29-5 And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:
We previously identified a pyridomorphinan (6, SRI-22138) possessing a 4-chlorophenyl substituent at the 5′-position on the pyridine and a 3-phenylpropoxy at the 14-position of the morphinan as a mixed μ opioid receptor (MOR) agonist and δ/κ opioid receptor (DOR/KOR) antagonist with potent antinociceptive activity and diminished tolerance and dependence in rodents. Structural variations at the 5′- and 14-positions of this mol. gave insights into the structure-activity relationships for binding and functional activity. Subtle structural changes exerted significant influence, particularly on the ability of the compounds to function as agonists at the MOR. In vivo evaluation identified compound 20(I) (SRI-39067) as a MOR agonist/DOR antagonist that produced systemically active potent antinociceptive activity in tail-flick assay in mice, with diminished tolerance, dependence/withdrawal, reward liability, and respiratory depression vs. morphine. These results support the hypothesis that mixed MOR agonist/DOR antagonist ligands may emerge as novel opioid analgesics with reduced side effects. The experimental part of the paper was very detailed, including the reaction process of 2-Pyridinylboronic acid(cas: 197958-29-5Related Products of 197958-29-5)
2-Pyridinylboronic acid(cas: 197958-29-5) belongs to pyridine. When pyridine is adsorbed on oxide surfaces or in porous materials, the following species are commonly observed: (i) pyridine coordinated to Lewis acid sites, (ii) pyridine H-bonded to weakly acidic hydroxyls, and (iii) protonated pyridine. At high coverage, physisorbed pyridine and protonated dimers can also be observed.Related Products of 197958-29-5